Antimicrobials V2 Flashcards

1
Q

Penicillin G is administed

A

IM or IV

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2
Q

Penicillin V is administed

A

orally

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3
Q

mechanism of penicillins

A

covalent binding to transpeptidases/PBPs, cross-linking, activation of autolysins

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4
Q

penicillins are bacterio-

A

cidal

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5
Q

block penicillin excretion with

A

probenecid

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6
Q

most ICWS inhibitors exibit

A

time dependent cell killing

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7
Q

clinical use: Pen G and Pen V

A

gram +

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8
Q

clinical use: anti-staphylococcal penicillins

A

beta-lactamase resistant

HHEELPSS
H. flu, H. pylori, E. coli, Enterococci, Listeria, Proteus mirabilis, Salmonella, Shigella

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9
Q

anti-staphylococcal penicillins

A

nafcillin, methicillin, isooxazolyl

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10
Q

extended spectrum antibiotics

A

ampicillin, amoxacillin

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11
Q

clinical use: extended spectrum penicillins

A

increased gram - activity

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12
Q

anti-pseudomonal penicillins

A

ticarcillin, piperacillin, mezlocillin

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13
Q

clinical use: anti-pseudomonal penicillins

A

effective against psuedomonas and some other gram -

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14
Q

due to rapid emergence of resistance with pseudomonas, use anti-psuedomonal penicillins in combination with

A

aminoglycosides or fluoroquinolones

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15
Q

adverse effects of penicillins

A

ampicillin rash
hypersensitivity: complete cross-linking
seizures w/ renal failure

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16
Q

resistance to penicillins

A

inaccessible PBPs (MRSA or gram -)
B-lactamase production

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17
Q

to reduced beta lactamase activity, administer penicillins with

A

b lactamase inhibitors

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18
Q

b lactamase inhibitors

A

clavulanic acid (augmenin)
sulbactam
tazobactam

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19
Q

clavulanic acid….

A

dramatically increases effects of pens

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20
Q

mechanism of cephalosporins

A

b-lactams, similar to pens

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21
Q

pen-sensitive patients may have cross reactivity with

A

cephalosporins

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22
Q

cephalosporins are bacterio

A

cidal

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23
Q

1st gen cephalosporins

A

cefazolin
cephalexin

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24
Q

2nd gen cephalosporins

A

cefuroxime
cefotetan
cefactor

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25
Q

3rd gen cephalosporins

A

ceftriaxone
cefotaxime
ceftazidime
cefpdoxime

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26
Q

4th gen cephalosporins

A

cefepime

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27
Q

cefepime exhibits _______ resistance

A

cephalosporinase

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28
Q

clinical use: 1st gen cephalosporins

A

gram +

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29
Q

clinical use: 2nd gen cephalosporins

A

some gram -, less gram +

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30
Q

clinical use: 3rd gen cephalosporins

A

serious gram - resistant to other b-lactams

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31
Q

clinical use: 4th gen cephalosporins

A

pseudomonas and cephalosporinase resistance

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32
Q

adverse effects: cephalosporins

A

irritation from injection
renal toxicity- enhanced by aminoglycosides
hypersensitivity
vitamin K deficiency

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33
Q

what antibiotics gives the Disulfiram effect?

A

cefotetan, bleeding and platelet disorders

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34
Q

what antibiotics gives the Disulfiram effect?

A

cefotetan, bleeding and platelet disorders

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35
Q

mechanism: azteronam

A

b lactam

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36
Q

clinical use: aztreonam

A

psuedomonas B-lactamase resistant

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37
Q

can azteronam cross the blood brain barrier?

A

yes

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38
Q

do azteronam exibit cross reactivity in pen-sensitive patients?

A

no

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39
Q

mechanism: imipenem

A

b lactam

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40
Q

clinical use: imipenem

A

broad, gram + and -

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41
Q

can imipenem cross the blood brain barrier?

A

yes

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42
Q

administration: imipenem

A

IV only

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43
Q

what should you coadminister with Imipenem?

A

cilastatin
inactivated by renal peptidase

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44
Q

meropenem

A

dipeptidase resistant carbapenem

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45
Q

does imipenem exhibit cross reactivity with pen-sensitive patients?

A

yes but incidence is low

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46
Q

mechanism: vancomycin

A

inhibits transglycosylation

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47
Q

vancomycin is bacteri-

A

cidal for gram +

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48
Q

vancomycin works synergistically with

A

aminoglycosides

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49
Q

vancomycin is given IV for

A

systemic use

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50
Q

vancomycin is given orally for

A

C. diff

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51
Q

clinical use: vancomycin

A

MRSA

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52
Q

adverse effects: vancomycin

A

flushing syndrome
renal and oto toxicity esp w/ aminoglycosides

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53
Q

mechanism: fosfomycin

A

inhibits cytoplasmic step in cell wall precursor synthesis
inhibits MurA blocking PG synthesis

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54
Q

clinical use: fosfomycin

A

gram + and gram -

single dose therapy UTI

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55
Q

fosfomycin is synergistic with

A

b lactams
aminoglycosides
fluoroquinolones

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56
Q

adverse effect: bacitracin

A

nephrotoxic

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57
Q

administration: bacitracin

A

topical only

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58
Q

pharmacokinetics: fosfomycin

A

G6P transporter

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59
Q

mechanism: colistin

A

act as detergents

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60
Q

clinical use: colistin

A

gram -

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61
Q

administation: colistin

A

topical due to renal toxicity

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62
Q

colistin is used as salvage therapy for

A

acinetobacter, pseudomonas, enterobacterieae

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63
Q

mechanism: tetracycline

A

reversible binding to 30S subunit

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64
Q

tetracycline is bacterio-

A

static

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65
Q

what class chelate metal ions?

A

tetracycline

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66
Q

what class should not be administered with calcium products?

A

tetracycline

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67
Q

can tetracyclines cross the placenta?

A

yes

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68
Q

excretion of doxycline

A

fecal

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69
Q

excretion of most tetracycline

A

urine

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70
Q

clinical use: tetracycline

A

broad spectrum
mycoplasma, chlamydia, rickettsiae
lyme disease

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71
Q

adverse effects: tetracycline

A

GI irritation
superinfections
liver damage
photosensitization
calcium chelation

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72
Q

resistance to tetracyclines

A

mainly efflux pumps
altered ribosomal proteins

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73
Q

glycycycline

A

newest tetracycline
retain antibacterial spectrum but overcome resistance

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74
Q

tigecycline is

A

not effected by efflux pump

75
Q

tigecycline comes with

A

FDA black box warning, very dangerous

76
Q

macrolides

A

erythromycin, clarithromycin, azithromycin

77
Q

do macrolides distribute to CNS?

A

no

78
Q

can macrolides cross the placenta?

A

yes

79
Q

excretion: macrolides

A

bile

80
Q

administration: macrolides

A

oral and IV

81
Q

clinical use: macrolides

A

gram +, some gram -

mycoplasma pneumoniae, legionnaire’s, chlamydia

82
Q

can macrolides be given to pen-sensitive patients?

A

yes

83
Q

broad spectrum macrolides

A

azithromycin and clarithromycin

84
Q

adverse effects: macrolides

A

GI distress
microsomal enzyme inhibition
hepatotoxicity
QT prolongation

85
Q

resistance: macrolides

A

staph resistant

methylated rRNA
efflux pump
esterase

86
Q

benefits of clarithromycin

A

less GI effects
longer half life

87
Q

which macrolide has minimal P450 interactions?

A

azithromycin

88
Q

clarithromycin and azithromycin have

A

better bioavailability
active against mycobacterium avium

89
Q

mechanism: telithromycin

A

binds 50S subunit

90
Q

pharmacokinetics: telithromycin

A

poor substrate for efflux
inhibits CYP3A4

91
Q

excretion: telithromycin

A

bile and urine

92
Q

clinical use: telithromycin

A

RTIs

93
Q

adverse effects: telithromycin

A

PQ prolongation

94
Q

mechanism: aminoglycosides

A

irreversible inactivation of 30S

95
Q

administration: aminoglycosides

A

usually IV

96
Q

where do aminoglycosides NOT distribute?

A

eye, CNS

97
Q

aminoglycosides and fluoroquinolones exhibit

A

concentration dependent killing

98
Q

clinical uses: aminoglycosides

A

gram -

99
Q

aminoglycosides for psuedomonas

A

gentamycin –> tobramycin –> amikacin

**oldest to newest

100
Q

older aminoglycosides

A

streptomycin, gentamycin

101
Q

adverse effects: aminoglycosides

A

nephrotoxicity
ototoxicity
dose and time dependent

102
Q

resistance: aminoglycosides

A

evolves rapidly if AG is used alone

increased bacterial metabolism
alteration in bacterial uptake
altered ribosomal target

103
Q

mechanism: chloramphenicol

A

reversible inhibitor of protein synthesis

104
Q

chloramphenicol is bacterio

A

static

105
Q

does chloarmphenicol distribute to the CNS?

A

yes

106
Q

excretion: chloramphenicol

A

urine

107
Q

resistance: chloramphenicol

A

plasmid mediated
CAT
slow development

108
Q

adverse effects: chloramphenicol

A

GI upset
anemia due to bone marrow depression
aplastic anemia (Irreversible and fatal)
Gray baby syndrome
inhibits CYP450

109
Q

clindamycin is bacterio

A

static

110
Q

mechanism: clindamycin

A

binds 50S subunit

111
Q

does clindamycin distribute to the CNS?

A

no

112
Q

clinical use: clindamycin

A

MRSA, endocarditis prophylaxis

113
Q

adverse effects: clindamycin

A

GI upset, C. diff, superinfections, hepatotoxicity

114
Q

streptogramins

A

quinupristin, dalfopristin

115
Q

mechanism: streptogramins

A

peptide macrolactones- bind novel ribosomal subunits

116
Q

administation: streptogramins

A

IV

117
Q

excretion: streptogramins

A

mostly bile, some urine

118
Q

streptogramins inhibit

A

CYP34A

119
Q

clinical use: streptogramins

A

vancomycin and MDR MRSA

120
Q

resistance: streptogramins

A

complete cross resistance between the two components

121
Q

mechanism: linezolid

A

prevents formation of 70S ribosome

122
Q

administration: linezolid

A

IV or oral

123
Q

clinical use: linezolid

A

bactericidal against streptococci
bacteriostatic against staphylococci and enterococci

vancomycin resistant e. faecium
limited to MDR gram+

124
Q

adverse effects: linezolid

A

bone marrow suppression, thrombocytopenia

125
Q

mechanism: sulfonamides

A

inhibit folate synthesis, PABA analogs

126
Q

sulfonamides are bacterio

A

static

127
Q

administration: sulfonamides

A

oral

128
Q

are sulfonamides distributed to the CNS?

A

yes

129
Q

excretion: sulfonamides

A

urine

130
Q

topical sulfonamide for burns

A

silver sulfadizine

131
Q

sulfonamide for ulcerative colitis

A

sulfasalazine

132
Q

sulfonamide for ulcerative colitis

A

sulfasalazine

133
Q

combine sulfonamides with

A

trimethoprim

134
Q

adverse effects: sulfonamides

A

allergic reactions
cross reaction with other sulfonamides
Stevens Johnson syndrome
hematuria

135
Q

resistance: sulfonamides

A

too much PABA
loss of permeability
new form of dihydropteroate synthesis

136
Q

mechanism: trimethoprim

A

block bacterial enzyme that converts dihydrofolate reductase to tetrahydrofolate

137
Q

adverse effects: trimethoprim

A

megaloblastic anemia
leukopenia
granulocytopenia

138
Q

co-trimoxazole

A

add typical sulfonamide effectds

139
Q

AIDS patients treat for pneumocystits receiving co-trimoxazole have

A

higher incidence of adverse effects

140
Q

mechanism: Fluoroquinolones

A

DNA gyrase inhibitors
topo II and topo IV

141
Q

fluoroquinolones

A

ciprofloxacin, levofloxacin

142
Q

fluoroquinolones excretion is blocked by

A

probenecid

143
Q

clinical use: fluoroquinolones

A

gram -, esp GI and UTI

144
Q

adverse effects: fluoroquinolones

A

GI upset
connective tissue disorder
headaches, dizziness, insomnia
abnormal LFTs

145
Q

resistance: fluoroquinolones

A

mutated DNA gyrase
plasmid-mediated protection
decreased permeability

146
Q

Nitrofurantoin

A

UTIs
no systemic effect, excreted in urine

147
Q

adverse effects: nitrofurantoin

A

anorexia
GI upset
hemolytic anemia

148
Q

resistance: nitrofurantoin

A

psuedomonas

149
Q

isoniazid mechanism

A

blocks synthesis of mycolic acid cell wall

150
Q

can isoniazid distribute to the CNS?

A

yes

151
Q

isoniazid metabolism

A

slow acetylators

152
Q

clinical use: isoniazid

A

prophylaxis: TB
combination therapy for TB with IPE

153
Q

adverse effects: isoniazid

A

dose and duration dependent
hepatotoxicity
peripheral and central neuropathy (B6)

154
Q

resistance: isoniazid

A

mutation of KatG gene

155
Q

mechanism: rifampin

A

inhibits DNA dependent RNA polymerase

156
Q

rifampin is bacterio

A

cidal

157
Q

excretion: rifampin

A

bile

158
Q

adverse effects: rifampin

A

induced of microsomal enzymes
hepatotoxic
flu-like syndrome

159
Q

mechanism: ethambutol

A

inhibits synthesis of mycobacterial and cell wall glycan via blocking arabinosyltransferase

160
Q

is ethambutol distributed to CNS?

A

yes

161
Q

excretion: ethambutol

A

urine

162
Q

adverse effects: ethambutol

A

dose dependent
optic neuritis, color blindess

163
Q

resistance: ethambutol

A

rapid, use in combination

164
Q

pyrazinamide is bacterio

A

static

165
Q

mechanism: pyrazinamide

A

activated by mycobacterium, blocks membrane functions

166
Q

resistance: pyrazinamide

A

rapid, use in combination

167
Q

adverse effects: pyrazinamide

A

hyperuricemia-gout
hepatotoxicity
contraindicated in pregnancy

168
Q

second line TB drugs

A

extreme cases
PAS, cycloserine, ethionamide

169
Q

dapsone

A

leprosy, p. jirovecii

170
Q

hepatotoxicity ICE T

A

Isoniazid
Clindamycin
Erythromycin
Tetracycline

171
Q

Ototoxicity: VA

A

vancomycin
aminoglycosides

172
Q

renal toxicity: CAVS

Cavities in Kidneys

A

cephalosporins
aminoglycosides
vancomycin
sulfonamides

173
Q

DOC H. flu

A

3rd gen cephalosporin

174
Q

DOC rickettsia/lyme disease

A

doxycycline

175
Q

DOC legionella

A

erythromycin, macrolides

176
Q

DOC m. tuberculosis

A

RIPE

177
Q

DOC M. pneumoniae

A

macrolides

178
Q

DOC C. diff

A

vancomycin

179
Q

pneumonia outpatient therapy healthy adults without risk

A

doxycycline, amoxicillin

***macrolide monotherapy (z pack) no longer recommended for S. pneumoniae

180
Q

pneumonia outpatient therapy adults with risk factors

A

amoxicillin/clavulanate OR

cephalosporin AND macrolide or doxycycline OR

fluoroquinolone alone

181
Q

pneumonia inpatient therapy no risk factors

A

ampicillin sulbactam OR

cephalosporin and macrolide OR

fluroquinolone alone

182
Q

pneumonia inpatient therapy, no risk factor BUT contraindication to macrolides and fluoroquinolones

A

beta lactam OR cephalosporin

AND doxycycline

183
Q

pneumonia inpatient therapy, risk for MRSA

A

vancomycin, linezolid

184
Q

pneumonia inpatient therapy, risk for Psuedomonas

A

piperacillin tazobactam

cefepime or carbapenems